Small-molecule inhibitors targeting Polycomb repressive complex 1 RING domain

June 21st, 2021 by Shirish Shukla

Nature Chemical Biology, Published online: 21 June 2021; doi:10.1038/s41589-021-00815-5

Fragment screening and medicinal chemistry optimization led to development of a small-molecule inhibitor of RING1B–BMI1 E3 ligase, blocking the H2A ubiquitination activity of the Polycomb repressive complex 1 and inducing differentiation in leukemia cells.
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